title: A novel flavonoid isolated from Sophora flavescens exhibited anti-angiogenesis activity, decreased VEGF expression and caused G0/G1 cell cycle arrest in vitro.
abstract: Kushen, the dried root of Sophora flavescens Ait, is a traditional Chinese herbal medicine. Kushen alkaloids have been developed in China as anticancer drugs, and more potent antitumor activities have been identified in kushen flavonoids than in kushen alkaloids. In this study, the anti-angiogenic properties of (2S)-7,2',4'-triihydroxy-5-methoxy-8-dimethylallyl flavanone (Compound 1, a novel flavonoid isolated from Kushen), were examined using the human umbilical vein endothelial cell line (ECV304) in vitro. The results indicated that compound 1 shows anti-angiogenesis activity via inhibitory effects on cell proliferation, cell migration, cell adhesion, and tube formation. Further studies indicated that compound 1 blocks cell cycles in the G0/G1 phase without inducing apoptosis, and down regulates vascular endothelial growth factor (VEGF) expression. The free radical scavenging activity of compound 1 was found through 2',7'-dichlorofluorescin diacetate (DCFH-DA) incubation assay in cells. The anti-angiogenic properties of compound 1 and its antiproliferative effect on endothelial cells without causing apoptosis make it a good candidate for development as a agent against development of tumors.
authors.affiliation: School of Life Sciences, Lanzhou University, Lanzhou, China.
authors.forename: Xiu-Li
authors.initials: XL
authors.lastname: Zhang
authors.forename: Mei-Ai
authors.initials: MA
authors.lastname: Cao
authors.forename: Li-Ping
authors.initials: LP
authors.lastname: Pu
authors.forename: Shuang-Sheng
authors.initials: SS
authors.lastname: Huang
authors.forename: Qing-Xiang
authors.initials: QX
authors.lastname: Gao
authors.forename: Cheng-Shan
authors.initials: CS
authors.lastname: Yuan
authors.forename: Chun-Ming
authors.initials: CM
authors.lastname: Wang
mesh_terms: D020533:Angiogenesis Inhibitors / Q000494:pharmacology*; D000975:Antioxidants / Q000494:pharmacology; D002448:Cell Adhesion / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D002460:Cell Line; D002465:Cell Movement / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004365:Drugs, Chinese Herbal; D042783:Endothelial Cells / Q000187:drug effects; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology*; D016193:G1 Phase / Q000187:drug effects*; D006801:Humans; D008870:Microtubules / Q000187:drug effects; D018517:Plant Roots / Q000737:chemistry; D017382:Reactive Oxygen Species / Q000378:metabolism; D016192:Resting Phase, Cell Cycle / Q000187:drug effects*; D029909:Sophora / Q000737:chemistry*; D042461:Vascular Endothelial Growth Factor A / Q000096:biosynthesis*
chemical_list: D020533:Angiogenesis Inhibitors; D000975:Antioxidants; D004365:Drugs, Chinese Herbal; D005419:Flavonoids; D017382:Reactive Oxygen Species; D042461:Vascular Endothelial Growth Factor A